Synthesis, biological assessment and molecular modeling of new dihydroquinoline-3-carboxamides and dihydroquinoline-3-carbohydrazide derivatives as cholinesterase inhibitors, and Ca channel antagonists
Tomassoli I.,Laboratoire Of Chimie Therapeutique Equipe 2Sbp Ea4267 |
Ismaili L.,Laboratoire Of Chimie Therapeutique Equipe 2Sbp Ea4267 |
Pudlo M.,Laboratoire Of Chimie Therapeutique Equipe 2Sbp Ea4267 |
De Los Rios C.,University of Alcalá |
And 7 more authors.
European Journal of Medicinal Chemistry | Year: 2011
The synthesis, biological evaluation, and molecular modeling of new 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamides(4), 4-hydroxy-2-oxo-1,2- dihydroquinoline-3-carbohydrazide (6), and some hexahydropyrimido[5,4-c] quinoline-2,5-diones (9) produced earlier by our laboratory, as AChE/BuChE inhibitors, is described. From these analyses compound 4c resulted equipotent regarding the inhibition of cholinesterases'; inhibitors 6k, 9a, 9b were selective for AChE, whereas product 4d proved selective for BuChE. Docking analysis has been carry out in order to identify the binding mode in the active site, and to explain the observed selectivities. Only compound 9a has been shown to decrease K+-induced calcium signals in bovine chromaffin cells.